Sequence-selective binding of C8-conjugated pyrrolobenzodiazepines (PBDs) to DNA

Mohammad A. Basher, Khondaker Miraz Rahman, Paul J.M. Jackson, David E. Thurston, Keith R. Fox

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5 Citations (Scopus)
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DNA footprinting and melting experiments have been used to examine the sequence-specific binding of C8-conjugates of pyrrolobenzodiazepines (PBDs) and benzofused rings including benzothiophene and benzofuran, which are attached using pyrrole- or imidazole-containing linkers. The conjugates modulate the covalent attachment points of the PBDs, so that they bind best to guanines flanked by A/T-rich sequences on either the 5′- or 3′-side. The linker affects the binding, and pyrrole produces larger changes than imidazole. Melting studies with 14-mer oligonucleotide duplexes confirm covalent attachment of the conjugates, which show a different selectivity to anthramycin and reveal that more than one ligand molecule can bind to each duplex.
Original languageEnglish
Pages (from-to)53-61
JournalBiophysical Chemistry
Early online date1 Sept 2017
Publication statusPublished - Nov 2017


  • Conjugate
  • Anthramycin
  • PBD
  • Polyamide
  • Footprinting
  • DNA melting


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